Publications & Patents

706. Synthesis of Functionalized Maoecrystal V Core Structures, K.C. Nicolaou, L. Dong, L. Deng, A.C. Talbot, D.Y.-K. Chen, Chem. Commun. 2010, 46, 70–72.

707. Cell Volume Decrease as a Link Between Azaspiracid-Induced Cytotoxicity and c-jun-N-Terminal Kinase Activation in Cultured Neurons, C. Vale, K.C. Nicolaou, M.O. Frederick, M.R. Vieytes, L.M. Botana, Toxicol. Sci. 2010, 113, 158–168.

708. Involvement of Capsase Activation in Azaspiracid-Induced Neurotoxicity in Neocortical Neurons, Z. Cao, K.T. Lepage, M.O. Frederick, K.C. Nicolaou, T.F. Murray, Toxicol. Sci. 2010, 214, 323–334.

709. Total Synthesis of (+)-Echinopines A and B, K.C. Nicolaou, H. Ding, J.-A. Richard, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 3815–3118.

710. An Expedient Procedure for the Oxidative Cleavage of Olefinic Bonds with PhI(OAc)2, NMO, and Catalytic OsO4, K.C. Nicolaou, V.A. Adsool, C.R.H. Hale, Org. Lett. 2010, 12, 1552–1555.

711. Origins of Regioselectivity of Diels–Alder Reactions for the Synthesis of Bisanthraquinone Antibiotic BE-43472B, A.E. Haydon, J. Becker, Y.H. Lim, K.C. Nicolaou, K.N. Houk, J. Org. Chem. 2010, 75, 922–928.

712. Synthesis of the ABCDEFG Ring System of Maitotoxin, K.C. Nicolaou, R.J. Aversa, J. Jin, F. Rivas, J. Am. Chem. Soc. 2010, 132, 6855–6861.

713. Total Synthesis and Structural Revision of Vannusals A and B. Synthesis of the Originally Assigned Structure of Vannusal B, K.C. Nicolaou, A. Ortiz, H. Zhang, P. Dagneau, Lanver, A.; Jennings, M. P.; Arseniyadis, S.; Faraoni, R.; Lizos, D. E. J. Am. Chem. Soc. 2010, 132, 7138–7152.

714. Total Synthesis and Structural Revision of Vannusals A and B. Synthesis of the True Structures of Vannusals A and B, K.C. Nicolaou, A. Ortiz, H. Zhang, G. Guella, J. Am. Chem. Soc. 2010, 132, 7153–7176.

715. Total Synthesis and Biological Evaluation of the Resveratrol-Derived Polyphenol Natural Products Hopeanol and Hopeahainol A, K.C. Nicolaou, Q. Kang, T.R. Wu, C.S. Lim, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 7540–7548.

716. Total Synthesis of Englerin A, K.C. Nicolaou, Q. Kang, S.Y. Ng, D.Y.-K. Chen, J. Am. Chem. Soc. 2010, 132, 8219–8222.

717. Total Synthesis and Structural Revision of Biyouyanagin B, K.C. Nicolaou, S. Sanchini, T.R. Wu, D. Sarlah, Chem. Eur. J. 2010, 16, 7678–7682.

718. Synthesis of the QRSTU Domain of Maitotoxin and Its 85-epi- and 86-epi-Diastereomers, K.C. Nicolaou, C.F. Gelin, J.H. Seo, Z. Huang, T. Umezawa, J. Am. Chem. Soc. 2010, 132, 9900–9907.

719. Asymmetric Total Synthesis of Cylindrocyclophanes A and F Through Cyclodimerization and a Ramberg–Bäcklund Reaction, K.C. Nicolaou, Y.-P. Sun, H. Korman, D. Sarlah, Angew. Chem. Int. Ed. 2010, 49, 5875–5878.

720. Total Synthesis of Sporolide B and 9-epi-Sporolide B, K.C. Nicolaou, J. Wang, Y. Tang, L. Botta, J. Am. Chem. Soc. 2010, 132, 11350–353.

721. Invigorating Education, K.C. Nicolaou, Angew. Chem. Int. Ed. 2011, 50, 63–74.

722. Synthesis of the C'D'E'F' Domain of Maitotoxin, K C. Nicolaou, J.H. Seo, T. Nakamura, R.J. Aversa, J. Am. Chem. Soc. 2011, 133, 214–219.

723. Synthesis of the WXYZA' Domain of Maitotoxin, K C. Nicolaou, T.M. Baker, T. Nakamura, J. Am. Chem. Soc. 2011, 133, 220–226.

724. Total Synthesis and Biological Evaluation of Monorhizopodin and 16-epi-Monorhizopodin, K.C. Nicolaou, X. Jiang, P.J. Lindsay-Scott, A. Corbu, S. Yamashiro, A. Bacconi, V.M. Fowler, Angew. Chem. Int. Ed. 2011, 50, 1139–1144.

725. Total Synthesis and Biological Evaluation of Marinopyrrole A and Analogs, K.C. Nicolaou, N.L. Simmons, J.S. Chen, N.M. Haste, V. Nizet, Tetrahedron Lett. 2011, 52, 2041–2043.

726. Maitotoxin: An Inspiration for Synthesis, K.C. Nicolaou, R.J. Aversa, Isr. J. Chem. 2011, 51, 359–377.

727. Design, Synthesis and Biological Evaluation of a Biyouyanagin Library, K.C. Nicolaou, S. Sanchini, D. Sarlah, G. Lu, D.K. Nomura, B.F. Cravatt, B. Cubitt, J.C. de la Torre, A.J. Hessell, D.R. Burton, Proc. Natl. Acad. Sci. U.S.A. 2011, 108, 6715–6720.

728. Addressing the Stereochemistry of Complex Organic Molecules by Density Functional Theory-NMR: Vannusal B in Retrospective, G. Saielli, K.C. Nicolaou, A. Ortiz, H. Zhang, A. Bagno, J. Am. Chem. Soc. 2011, 133, 6072–6077.

729. An Expedient Synthesis of a Functionalized Core Structure of Bielschowskysin, K.C. Nicolaou, V.A. Adsool, C.R.H. Hale, Angew. Chem. Int. Ed. 2011, 50, 5149–5152.

730. Enantioselective Dichlorinatoin of Allylic Alcohols, K.C. Nicolaou, N.L. Simmons, Y. Ying, P.M. Heretsch, J.S. Chen, J. Am. Chem. Soc. 2011, 133, 8134–8137.

731. Total Synthesis of Epicoccin G, K.C. Nicolaou, S. Totokotsopoulos, D. Giguère, Y. Sun, D. Sarlah, J. Am. Chem. Soc. 2011, 133, 8150–8153.

732. Proteomic Signature of Fatty Acid Biosynthesis Inhibition Available for In Vivo Mechanism of Action Studies, M. Wenzel, M Patra, D. Alrecht, D.Y.-K. Chen, K.C. Nicolaou, N. Metzler-Nolte, J.E. Bandow, Antimicrob. Agents Chemother. 2011, 55, 2590–2596.

733. Synthesis of the Carboline Disaccharide Domain of Shishijimicin A, K.C. Nicolaou, J.L. Kiappes, W. Tian, V.B. Gondi, J. Becker, Org. Lett. 2011, 13, 3924–3927.

734. Sulfonamides as a New Scaffold for Hypoxia Inducible Factor Pathway Inhibitors, C. Tan, R. de Noronha, N.S. Devi, A.A. Jabbar, S. Kaluz, Y.Liu, S. Reid Mooring, K.C. Nicolaou, B. Wang, E.G. Van Meir, Bioorg. Med. Chem. Lett. 2011, 21, 5528–5532.

735. Synthesis and Biological Evaluation of 2',4'- and 3',4'-Bridged Nucleoside Analogues, K.C. Nicolaou, S.P. Ellery, F. Rivas, K. Saye, E. Rogers, T.J. Workinger, M. Schallenberger, R. Tawatao, A. Montero, A. Hessell, F. Romesberg, D. Carson, D. Burton, Bioorg. Med. Chem. 2011, 19, 5648–5669.

736. Bioinspired Synthesis of Hirsutellones A, B and C, K.C. Nicolaou, Y.-P. Sun, D. Sarlah, W. Zhan, T.R. Wu, Org. Lett. 2011, 13, 5707–5710.

737. A Practical Sulfenylation of 2,5-Diketopiperazines, K.C. Nicolaou, D. Giguère, S. Totokotsopoulos, Y.-P. Sun, Angew. Chem. Int. Ed. 2012, 51, 728–732.

738. Synthesis of Macroheterocycles through Intramolecular Oxidative Coupling of Furanoid b-Ketoesters, K.C. Nicolaou, C.R.H. Hale, C. Ebner, C. Nilewski, C.F. Ahles, D. Rhoades, Angew. Chem. Int. Ed. 2012, 51, 4726–4730.

739. Bio-inspired Synthesis and Biological Evaluation of a Colchicine-related Compound Library, K.C. Nicolaou, R.A. Valiulin, J.K. Pokorski, V. Chang, J.S. Chen, Bioorg. Med. Chem. Lett. 2012, 22, 3776–3780.

740. Total Syntheses of Anominine and Tubingensin A, M. Bian, Z. Wang, X. Xiong, Y. Sun, C. Matera, K.C. Nicolaou, A. Li, J. Am. Chem. Soc. 2012, 134, 8078–8081.

741. Constructing Molecular Complexity and Diversity: Total Synthesis of Natural Products of Biological and Medicinal Importance, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, H.A. Ioannidou, Chem. Soc. Rev. 2012, 41, 5185–5238.

742. A Total Synthesis Trilogy: Calicheamicin γ1I, Taxol, and Brevetoxin A, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, Chem. Rec. 2012, 12, 407–441.

743. Aldehyde Dehydrogenase Inhibitors: A Comprehensive Review of the Pharmacology, Mechanism of Action, Substrate Specificity, and Clinical Application, V. Koppaka, D.C. Thompson, Y. Chen, M. Ellermann, K.C. Nicolaou, R.O. Juvonen, D. Petersen, R.A. Deitrich, T.D. Hurley, V. Vasiliou, Pharmacol. Rev. 2012, 64, 520–539.

744. Synthesis and Biological Evaluation of Epidithio-, Epitetrathio- and bis-(Methylthio)diketopiperazines: Synthetic Methodology, Enantioselective Total Synthesis of Epicoccin G, 8,8'-epi-ent-Rostratin B, Gliotoxin, Gliotoxin G, Emethallicin E and Haematocin and Discovery of New Antiviral and Antimalarial Agents, K.C. Nicolaou, M. Lu, S. Totokotsopoulos, P. Heretsch, D. Giguère, Y. Sun, D. Sarlah, T.H. Nguyen, I.C. Wolf, D.F. Smee, C.W. Day, S. Bopp, E.A. Winzeler, J. Am. Chem. Soc. 2012, 134, 17320–17332.

745. Arylsulfonamide KCN1 Inhibits In Vivo Glioma Growth and Interferes with HIF Signaling by Disrupting HIF-1α Interaction with Cofactors p300/CBP, S. Yin, S. Kaluz, N.S. Devi, A.A. Jabbar, R.G. de Noronha, J. Mun, Z. Zhang, P.R. Boreddy, W. Wang, Z. Wang, T. Abbruscato, Z. Chen, J.J. Olson, R. Zhang, M.M. Goodman, K.C. Nicolaou, E.G. Van Meir, Clin. Cancer Res. 2012, 18, 6623–6633.

746. How Thiostrepton Was Made in the Laboratory, K.C. Nicolaou, Angew. Chem. Int. Ed. 2012, 51, 12414–12436.

747. The Emergence of the Structure of the Molecule and the Art of Its Synthesis, K.C. Nicolaou, Angew. Chem. Int. Ed. 2013, 52, 131–146.

748. General Synthetic Approach to Functionalized Dihydrooxepines, K.C. Nicolaou, R. Yu, L. Shi, Q. Cai, M. Lu, P. Heretsch, Org. Lett. 2013, 15, 1994–1997.

749. Synthesis and Biological Evaluation of New Paclitaxel Analogs and Discovery of Potent Antitumor Agents, K.C. Nicolaou, R.A. Valiulin, Org. Biomol. Chem. 2013, 11, 4154–4163.

750. Total Synthesis and Structural Revision of Viridicatumtoxin B, K. C. Nicolaou, C. Nilewski, C. R. H. Hale, H. A. Ioannidou, A. ElMarrouni, L. G. Koch, Angew. Chem. Int. Ed. 2013, 52, 8736–8741.

751. Synthesis and Antioxidation Evaluation of (S,S)- (R,R)-Secoisolariciresinal Diglucosides (SDGs), O.P. Mishra, N. Simmons, S. Tyagi, R. Pietrofesa, V.V. Shuvaev, R.A. Valiulin, P. Heretsch, K.C. Nicolaou, M. Christofidou-Solomidou, Bioorg. Med. Chem. Lett. 2013, 23, 5325–5328.

752. Microsphere-based Immunoassay for the Detection of Azaspiracids, L.P. Rodríguez, N. Vilariño, M.C. Louzao, T.J. Dickerson, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Anal. Biochem. 2014, 447, 58–63.

753. In Vivo Arrhythmogenicity of the Marine Biotoxin Azaspiracid-2 in Rats, S.F. Ferreiro, N. Vilariño, C. Carrera, M.C. Louzao, G. Santamarina, A.G. Cantalapiedra, L.P. Rodríguez, J.M. Cifuentes, A.C. Vieira, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Arch. Toxicol. 2014, 88, 425–434.

754. Organic Synthesis: The Art of Replicating the Molecules of Living Nature and Others Like Them in the Laboratory, K.C. Nicolaou, Proc. Royal Soc. A 2014, 470, 20130690.

755. Cyclic Marinopyrrole Derivatives as Disruptors of Mcl-1 and Bcl-xL Binding to Bim, C. Cheng, Y. Liu, M. E. Balasis, N. L. Simmons, J. Li, H. Song, L. Pan, Y. Qin, K. C. Nicolaou, S. M. Sebti, R. Li, Mar. Drugs 2014, 12, 1335-1348.

756. The Endeavor of Total Synthesis and Its Impact on Chemistry, Biology, and Medicine, K.C. Nicolaou, C.R.H. Hale, Natl. Sci. Rev. 2014, 1, 233-252.

757. Academic–Industrial Partnerships in Drug Discovery and Development, K.C. Nicolaou, Angew. Chem. Int. Ed. 2014, 53, 4730-4731.

758. Marinopyrrole Derivatives with Sulfide Spacers as Selective Disruptors of Mcl-1 Binding to Pro-Apoptotic Protein Bim, C. Cheng, Y. Liu, M.E. Balasis, T.P. Garner, J. Li, N.L. Simmons, N. Berndt, H. Song, L. Pan, Y. Qin, K.C. Nicolaou, E. Gavathiotis, S.M. Sebti, R. Li. Mar. Drugs 2014, 12, 4311–4325.

759. Advancing the Drug Discovery and Development Process, K.C. Nicolaou, Angew. Chem. Int. Ed. 2014, 53, 9128–9140.

760. Total Synthesis of Viridicatumtoxin B and Analogues Thereof: Stretegy Evolution, Structural Revision, and Biological Evaluation, K.C. Nicolaou, C.R.H. Hale, C. Nilewski, H.A. Ioannidou, A. ElMarrouni, L.G. Nilewski, K. Beabout, T.T. Wang, Y. Shamoo, J. Am. Chem. Soc. 2014, 136, 12137–12160.

761. Total Synthesis of Δ12-Prostaglandin J3, a Highly Potent and Selective Antileukemic Agent, K.C. Nicolaou, P. Heretsch, A. ElMarrouni, C.R.H. Hale, K.K. Pulukuri, A.K. Kudva, V. Narayan, K.S. Prabhu, Angew. Chem. Int. Ed. 2014, 53, 10443–10447.

762. Total Synthesis of Myceliothermophins C, D and E, K.C. Nicolaou, L. Shi, M. Lu, M.R. Pattanayak, A.A. Shah, H.A. Ioannidou, M. Lamani, Angew. Chem. Int. Ed. 2014, 53, 10970–10974.

763. The Chemistry–Biology–Medicine Continuum and the Drug Discovery and Development Process in Academia, K.C. Nicolaou, Chem. Biol. 2014, 21, 1039–1045.

764. In Vitro Chronic Effects on hERG Channel Caused by the Marine Biotoxin Azaspiracid-2, S.F. Ferreiro, N. Vilariño, M.C. Louzao, K.C. Nicolaou, M.O. Frederick, L.M. Botana, Toxicon 2014, 78, 69–75.

765. Organic Synthesis, K.C. Nicolaou, C. Nilewski, in Discoveries in Modern Science: Exploration, Invention, Technology, J. Trefil, Ed., eBook, Macmillan Reference USA, MI, 2014.

766. Synthesis and Biological Evaluation of QRSTUVWXYZA′ Domains of Maitotoxin, K.C. Nicolaou, P. Heretsch, T. Nakamura, A. Rudo, M. Murata, K. Konoki, J. Am. Chem. Soc. 2014, 136, 16444–16451.

767. Total Synthesis of Trioxacarcin DC-45-A2, K.C. Nicolaou, Q. Cai, B. Qin, M.T. Peterson, R.J.T. Mikkelsen, P. Heretsch, Angew. Chem. Int. Ed. 2014, 53, in press.

768. Synthesis and Biological Evaluation of Dimeric Furanoid Macroheterocycles: Discovery of New Anticancer Agents, K. C. Nicolaou, C. Nilewski, C. R. H. Hale, C. F. Ahles, C. A. Chiu, C. Ebner, A. ElMarrouni, L. Yang, K. Stiles, D. Nagrath, J. Am. Chem. Soc. 2015, 137, 4766–4770.

769. Total Synthesis and Structural Revision of Antibiotic CJ-16,264, K. C. Nicolaou, A. A. Shah, H. Korman, T. Khan, L. Shi, W. Worawalai, E. A. Theodorakis, Angew. Chem. Int. Ed. 2015, 54, 9203-9208.

770. Total Synthesis of Shishijimicin A, K. C. Nicolaou, Z. Lu, R. Li, J. R. Woods, T. Sohn, J. Am. Chem. Soc. 2015, 137 (27), 8716–8719.

771. Practical Synthesis of p- and o-Amino- and Methoxyphenolic Anthraquinones, K. C. Nicolaou, M. Lu, P. Chen, and A. A. Shah, Angew. Chem. Int. Ed. 2015, 54, 12687-12691.

772. Synthesis and Biological Evaluation of Novel Epothilone B Side Chain Analogues, K. C. Nicolaou, D. Rhoades, Y. Wang, S. Totokotsopoulos, R. Bai, E. Hamel, ChemMedChem 2015. DOI: 10.1002/cmdc.201500401.

773. Synthesis and Biopharmaceutical Evaluation of Imatinib Analogues Featuring Unusual Structural Motifs, K. C. Nicolaou, D. Vourloumis, S. Totokotsopoulos, A. Papakyriakou, H. Karsunky, H. Fernando, J. Gavrilyuk, D. Webb, A. F. Stepan, ChemMedChem 2015. DOI: 10.1002/cmdc.201500510.

774. Total Synthesis and Biological Evaluation of Natural and Designed Tubulysins, K. C. Nicolaou, D. Mandal, P. Klahn, J. Yin, M. Jin, R. D. Erande, J. Gavrilyuk, D. Vourloumis, 2015, submitted.

775. Total Synthesis of Trioxacarcins DC-45-A1, A, D, C and C7"-epi-C and Full Structural Assignment of Trioxacarcin C, K. C. Nicolaou, Q. Cai, 2015, submitted.

776. Synthesis and Biological Investigation of 12-Prostaglandin J3 (12-PGJ3) Analogues and Related Compounds, K.C. Nicolaou, K.K. Pulukuri, S. Rigol, P. Heretsch, R. Yu, C.I. Grove, C.R.H. Hale, A. ElMarrouni, V. Fetz, M. Brönstrup, M. Aujay, J. Sandoval, J. Gavrilyuk, J. Am. Chem. Soc. 2016, 138, 6550–6560.

777. Efficient Synthesis of Dimeric Oxazoles, Piperidines and Tetrahydroisoquinolines from N-Substituted 2-Oxazolones, Y. He, P.K. Agarwal, I.N. Chaithanya Kiran, R. Yu, B. Cao, C. Zou, X. Zhou, H. Xu, B. Xu, L. Zhu, Y. Lan, K.C. Nicolaou, Chem. Eur. J. 2016, 22, 7696–7701.

778. Total Synthesis of 12-Prostaglandin J3 and Related Prostanoids: Evolution of Synthetic Strategies to a Streamlined Process, K.C. Nicolaou, K.K. Pulukuri, R. Yu, S. Rigol, P. Heretsch, C.I. Grove, C.R.H. Hale, A. ElMarrouni, Chem. Eur. J. 2016, 22, 8559–8570.

779. Total Synthesis of Thailanstatin A, K.C. Nicolaou, D. Rhoades, M. Lamani, M.R. Pattanayak, S. Mothish Kumar, J. Am. Chem. Soc. 2016, 138, 7532–7535.

780. Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations, K.C. Nicolaou, Y. Wang, M. Lu, D. Mandal, M.R. Pattanayak, R. Yu, A.A. Shah, J.S. Chen, H. Zhang, J.J. Crawford, L. Pasunoori, Y.B. Poudel, N.S. Chowdari, C. Pan, A. Nazeer, S. Gangwar, G. Vite, E.N. Pitsinos, J. Am. Chem. Soc. 2016, 138, 8235–8246.

781. Catalyst: Synthetic Organic Chemistry as a Force for Good, K.C. Nicolaou, Chem 2016, 1, 331–334.

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